• See Also
  1. Anti-Retroviral Therapy
  2. Nucleoside Reverse Transcriptase Inhibitor
  • Indications
  1. HIV Infection (Anti-Retroviral Therapy)
    1. Replaced by other more potent nRTI with less frequent dosing, and less severe adverse effects
  • Mechanism
  1. Nucleoside Reverse Transcriptase Inhibitor
  2. Inhibits HIV replication
  • Pharmacokinetics
  1. Well absorbed (87% oral Bioavailability)
  • Efficacy
  1. Replaced by other nRTIs with greater potency
  2. Combination treatment Zalcitabine and Zidovudine (AZT)
    1. Late HIV without prior Anti-Retroviral Therapy
    2. Large and sustained CD4 Count increase
    3. Improves survival in patients with late HIV disease
  • Dosing
  1. Zalcitabine 0.75 mg orally THREE times daily
  • Adverse Effects
  1. See nRTI for adverse effects attributed to the class
  2. More significant adverse effects than newer nRTI agents
  3. Common symptoms during the first several weeks
    1. Effects
      1. Maculovesicular cutaneous eruptions
      2. Mucosal Ulcers
      3. Fevers
    2. Symptoms often resolve without stopping medication
    3. Consider Symptomatic therapy
      1. Tylenol
      2. Antihistamines
      3. NSAIDS
    4. Symptoms less frequent at a dose of 2.25 mg/day
  4. Painful Sensorimotor leg Peripheral Neuropathy (10-25%)
    1. Major dose limiting toxicity
    2. Discontinue drug at first signs of Neuropathy!
    3. Symptoms usually resolve over a few weeks
  5. Pancreatitis (<1%)
  • References
  1. (1998) Med Lett Drugs Ther 40(1041):115 [PubMed]
  2. (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
  3. Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]